On December 8, 2018 Context Therapeutics, a clinical-stage biotechnology company, reported new preclinical data on Apristor (onapristone extended release), its first-in-class full progesterone receptor antagonist, showing that the investigational medicine inhibits tumor cell line growth in hormone receptor positive (HR+) breast cancer cell lines (Press release, Context Therapeutics, DEC 8, 2018, View Source [SID1234531939]). Additionally, it was shown that Apristor is synergistic with current standard of care therapies for HR+ metastatic breast cancer, including the Cdk4/6 inhibitor Ibrance (palbociclib) and the selective estrogen receptor degrader Faslodex (fulvestrant).
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"Progesterone receptor is the forgotten target", said Carol Lange, PhD, Professor of Medicine at the University of Minnesota and principal investigator of the research presentation. "HR+ breast cancer is driven by two hormones, estrogen and progesterone. While there are over half a dozen approved medicines to block estrogen and estrogen-related signaling, there are no FDA approved medicines in cancer to block progesterone. The data presented shows that blocking progesterone-related signaling via Apristor is not only active alone in tumor models but it also enhances the activity of medicines that either directly or indirectly target estrogen."
The data presented shows that:
Progesterone / progesterone peceptor (PR) is a unique target distinct from estrogen / estrogen receptor
PR is critical for in vitro growth of HR+ breast cancer cells
PR antagonism via Apristor reduces the expression of cancer promoting genes
PR antagonism is synergistic with Cdk4/6 inhibitors and a SERD
"We are encouraged by these new preclinical data, which speak to the important role PR plays in facilitating HR+ breast cancer disease progression," said Deepak Lala, PhD, Chief Technology Officer of Context. "This is the first study to show that PR antagonism is synergistic with new treatment modalities, including Cdk4/6 inhibition. "
About Apristor
Apristor (onapristone extended release) is Context’s wholly owned, first-in-class, orally active extended release formulation of onapristone, a full progesterone receptor antagonist. Progesterone receptor [PR] plays a critical role in facilitating breast cancer disease progression as well as therapeutic resistance to first line antiestrogen and/or Cdk4/6 inhibitor therapies. Apristor is the only full PR antagonist that is being developed to target breast cancer. Apristor has the potential to transform the treatment of breast cancer, through the potent inhibition of PR signaling thereby blocking breast cancer cell proliferation and overcoming resistance to first line antiestrogen and Cdk4/6 inhibitor therapy.